Batimastat (BB-94) sodium salt is a broad-spectrum MMP inhibitor (IC50s: 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7, and MMP-3).

MMP3:20 nM , MMP1:3 nM , MMP2:4 nM , MMP7:6 nM , MMP9:4 nM

Batimastat inhibits gelatinases A and B (IC50s: 4 nM and 10 nM). The IC50 with the structurally similar collagenase Ht-d is 6 nM, which is comparable with values for MMP-1 (3 nM), MMP-8 (10 nM), and MMP-3 (20 nM) [2]. CD30 shedding from the cell line Karpas299 can effectively be blocked by the hydroxamic acid-based metalloproteinase inhibitor Batimastat (IC50: 230 nM) [3].

Matrix density in animals treated with saline or Batimastat (40 mg/kg) is analyzed 4 hours post-E2 administration, a critical point when collagen density notably decreases following hormone treatment [6]. Batimastat intraperitoneally administers to restrict human ovarian carcinoma xenografts and murine melanoma metastasis, alongside delaying primary tumor growth in human breast cancer models without inducing cytotoxicity or affecting mRNA levels [2]. Exhibiting antineoplastic and antiangiogenic effects across tumor models, Batimastat's concomitant application with Cisplatin (60 mg/kg i.p. bi-daily for 8 injections and 4 mg/kg i.v. every 7 days for 3 injections, respectively) effectively halts growth and dissemination of xenografts, maintaining all subjects' health up to day 200 [4]. Furthermore, Kaplan-Meier survival analysis (48 hours) highlights a significant survival rate increase to 95.2% in Batimastat-treated animals versus 75% in controls, with statistical relevance nearing significance (p=0.064) [5].

6. Russo LA, et al. Regulated expression of matrix metalloproteinases, inflammatory mediators, and endometrial matrix remodeling by 17beta-estradiol in the immature rat uterus. Reprod Biol Endocrinol. 2009 Nov 4;7:124.

http://www.ncbi.nlm.nih.gov/pubmed/19889233